Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors

…, Y Wu, B Doughan, ZJ Jia, J Woolfrey, B Huang…

文献索引：Su, Ting; Wu, Yanhong; Doughan, Brandon; Jia, Zhaozhong J.; Woolfrey, John; Huang, Brian; Wong, Paul; Park, Gary; Sinha, Uma; Scarborough, Robert M.; Zhu, Bing-yan Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 22 p. 2947 - 2950

全文：HTML全文

被引用次数: 7

摘要

We have previously reported the design and synthesis of various dibasic fXa inhibitors using amino acids such as 3-OH-proline, m-amidinophenylalanine, and 2,3-diamino propionic acid as templates ( 1 in Fig. 1). 4 To discover novel inhibitors with improved bioavailability, we focused our synthetic efforts on reducing the overall basicity and enhancing the potency of this series of compounds. Quan et al. 5 has reported isoxazoline-containing fXa inhibitors (2 in Fig. ...